Abstract：
:Several novel γ-carboline derivatives were identified as selective inhibitors of bovine viral diarrhea virus (BVDV) replication in cell cultures. Among them, 3,4,5-trimethyl-γ-carboline (SK3M4M5M) was the most active against BVDV (Nose strain) in MDBK cells, with a 50% effective concentration of 0.017±0.005μM and a selectivity index of 435. The compound inhibited viral RNA synthesis in a dose-dependent fashion. In a time of drug-addition experiment during a single viral replication cycle, SK3M4M5M lost its antiviral activity when first added at 8h or later after infection, which coincides with the onset of viral RNA synthesis. When selected γ-carboline derivatives, including SK3M4M5M, were examined for their inhibitory effect on the mutant strains resistant to some classes of nonnucleoside BVDV RNA-dependent RNA polymerase inhibitors, all of which target the top of the finger domain of the polymerase, the strains displayed cross-resistance to the γ-carboline derivatives. These results indicate that the γ-carboline derivatives may possibly target a hot spot of the RNA-dependent RNA polymerase. Although SK3M4M5M was highly active against BVDV, the compound proved inactive against hepatitis C virus (HCV) in HCV RNA replicon cells.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Salim MT,Goto Y,Hamasaki T,Okamoto M,Aoyama H,Hashimoto Y,Musiu S,Paeshuyse J,Neyts J,Froeyen M,Herdewijn P,Baba Mdoi
10.1016/j.antiviral.2010.09.013subject
Has Abstractpub_date
2010-12-01 00:00:00pages
263-8issue
3eissn
0166-3542issn
1872-9096pii
S0166-3542(10)00735-7journal_volume
88pub_type
杂志文章abstract：:Infection with the oncogenic γ-herpesviruses Epstein-Barr virus (EBV) and Kaposi's sarcoma-associated herpesvirus (KSHV) cause several severe malignancies in humans. Inhibition of the lytic replication of EBV and KSHV eliminates the reservoir of persistent infection and transmission, consequently preventing the occurr...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.12.002
更新日期：2017-02-01 00:00:00
abstract：:Carbovir (CBV) is a guanine nucleoside analog with potent in vitro anti-HIV activity. A prodrug of CBV is currently being evaluated in clinical trials as a potential agent for the treatment of AIDS. The ability of CBV to inhibit mitochondrial DNA synthesis in intact CEM cells was evaluated in the present study, becaus...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(97)01033-4
更新日期：1997-05-01 00:00:00
abstract：:Respiratory syncytial virus (RSV) infection causes significant disease in the lower respiratory tract of young children, and there is currently no licensed vaccine to prevent RSV infection. The F glycoprotein is considered a major antigenic target for RSV vaccine development. Recent evidence indicates that the pre-fus...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.02.017
更新日期：2019-05-01 00:00:00
abstract：:Mycophenolate mofetil (MMF), a therapeutically used inhibitor of inosine monophosphate dehydrogenase is hydrolyzed to its active metabolite mycophenolic acid (MPA) in vivo. MPA exhibits anti-HIV activity in vitro. We tested MPA alone and in combination with abacavir (ABC), didanosine (DDI), lamivudine (3TC) and tenofo...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(02)00006-2
更新日期：2002-07-01 00:00:00
abstract：:3'-Azido-3'-deoxythymidine triphosphate (erythro) and its threo isomer were synthesized and investigated for their inhibition of HIV reverse transcriptase from virus isolate U 937/HTLV-III. The erythro isomer was a competitive inhibitor of the reaction directed by (rA)n(dT)12-18 and the Ki value was 0.0022 microM. The...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(87)90002-7
更新日期：1987-03-01 00:00:00
abstract：:The first 230 residues of the 298-amino acid glycoprotein G of respiratory syncytial virus (RSV) are sufficient to confer complete resistance to challenge with live RSV, whereas the first 180 residues completely failed (Olmsted et al. (1989) J. Virol. 63, 411-420). The characterization of a protective epitope correspo...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(95)00053-4
更新日期：1995-12-01 00:00:00
abstract：:Human cytomegalovirus (HCMV) infections cause congenital birth defects and disease in immunosuppressed individuals. Antiviral compounds can control infection yet their use is restricted due to concerns of toxicity and the emergence of drug resistant strains. We have evaluated the impact of an RNA Polymerase I (Pol I) ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2018.02.014
更新日期：2018-05-01 00:00:00
abstract：:Rabies is a lethal viral infection that can affect almost all mammals, including humans. To better understand the replication of Rabies lyssavirus, we investigated if the viral load in brains naturally infected with rabies influences viral internalization and viral growth kinetics in neuroblastoma cells, and if the vi...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.11.003
更新日期：2018-01-01 00:00:00
abstract：:Isoborneol, a monoterpene and a component of several plant essential oils, showed dual viricidal activity against herpes simplex virus 1 (HSV-1). First, it inactivated HSV-1 by almost 4 log10 values within 30 min of exposure, and second, isoborneol at a concentration of 0.06% completely inhibited viral replication, wi...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(99)00036-4
更新日期：1999-09-01 00:00:00
abstract：:Chronic hepatitis B infection remains a major public health problem worldwide. The hepatitis B virus belongs to the family of hepadnaviruses that replicate their DNA genome via a reverse transcription pathway. The chronicity of infection in infected hepatocytes is maintained by the persistence of the viral covalently ...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/s0166-3542(99)00056-x
更新日期：1999-11-01 00:00:00
abstract：:The prevention and control of disease caused by seasonal and potential pandemic influenza viruses is currently managed by the use influenza vaccines and antivirals. The adamantanes (amantadine and rimantadine) were the first antivirals licensed for use against influenza A viruses and have been used extensively in some...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.08.002
更新日期：2007-02-01 00:00:00
abstract：:This review describes the procedures for the use of fluorochrome labeled monoclonal antibodies and flow cytometry for the detection and quantification of virus infected cells. The application of this technology for (1) identifying virus infected cells in clinical specimens obtained from human cytomegalovirus (HCMV) an...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/s0166-3542(99)00039-x
更新日期：1999-08-01 00:00:00
abstract：:MicroRNA-122 (miR-122) is involved in the pathogenesis of several liver diseases, including chronic hepatitis B infection and hepatocellular carcinoma. This study aimed to explore the potential role of miR-122 in the interferon (IFN)-mediated suppression of hepatitis B virus (HBV) in hepatocytes. We found that elevate...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2015.03.001
更新日期：2015-06-01 00:00:00
abstract：:A series of phosphoramidate derivatives of the anti-HIV drug AZT has been prepared as membrane soluble pro-drugs of the bio-active nucleotide forms and evaluated in vitro against HIV-1. Terminal substituted alkyl amines have a pronounced anti-HIV effect: this effect declines upon increasing the length of the methylene...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(90)90053-a
更新日期：1990-12-01 00:00:00
abstract：:The reverse transcriptase (RT) of HIV which has been inhibited by the incorporation of AZT into the primer strand is subject to a deblocking reaction by cellular ATP. This reaction yields unblocked primer plus the dinucleoside tetraphosphate, AZTp(4)A. In the present study, we report that AZTp(4)A is an excellent subs...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(03)00003-2
更新日期：2003-05-01 00:00:00
abstract：:Despite the importance of Dengue virus (DENV) infection in human health, there is not a fully effective vaccine or antiviral treatment against the infection. Since lipids such as cholesterol are required during DENV infection, its uptake and synthesis are increased in infected cells. Ezetimibe is an FDA-approved drug ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2018.10.024
更新日期：2018-12-01 00:00:00
abstract：:SeqHepB is a combination of a HBV genome sequence analysis program and a relational database that houses data collected from multiple data sources. Registered users can access the sequence analysis component of SeqHepB online for rapid and detailed interrogation of HBV genomic sequences. Its main function is to determ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.11.014
更新日期：2007-07-01 00:00:00
abstract：:Tiazofurin (2-beta-D-ribofuranosylthiazole-4-carboxamide) was examined for its activity against tomato-spotted wilt virus (TSWV) in tomato plants. Solutions containing 50, 100, 200, 400 and 800 mg/l of the drug were sprayed onto the leaves. The results showed that 100 and 200 mg/l were the most efficient concentration...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(84)90003-2
更新日期：1984-12-01 00:00:00
abstract：:AIDS therapies employing HIV protease inhibitors (PIs) are associated with changes in fat metabolism. However, the cellular mechanisms affected by PIs are not clear. Thus, the affects of PIs on adipocyte differentiation were examined in vitro using C3H10T1/2 stem cells. In these cells the PIs, nelfinavir, saquinavir, ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(00)00102-9
更新日期：2000-08-01 00:00:00
abstract：:Oxymatrine (OMTR) is an anti-hepatitis drug used in China. Its mechanism of action is unknown. Recently, we found that OMTR inhibits hepatitis B virus (HBV) via down-regulating the expression of heat-stress cognate 70 (Hsc70), a host protein required for HBV DNA replication. Goal of this study was to assess the effect...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2011.01.005
更新日期：2011-03-01 00:00:00
abstract：:Foot-and-mouth disease virus (FMDV) causes a highly contagious disease of cloven-hoofed animals. We have reported (Cubillos et al., 2008) that a synthetic dendrimeric peptide consisting of four copies of a B-cell epitope [VP1(136-154)] linked through thioether bonds to a T-cell epitope [3A(21-35)] of FMDV [B4T(thi)] e...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.03.005
更新日期：2016-05-01 00:00:00
abstract：:EV71 is a major causative agent of hand, foot and mouth disease (HFMD) and is responsible for large outbreaks in various Asian Pacific countries. In the present study, we generated the recombinant baculovirus (Bac-VP1) encoding VP1 in a novel expression cassette. The transmembrane domain of hemagglutinin of the H3N2 i...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2012.05.017
更新日期：2012-09-01 00:00:00
abstract：:Crimean-Congo hemorrhagic fever (CCHF) is a tick-borne viral disease of humans that affects a wide geographic area of Africa and Eurasia, including Turkey, Iran, Pakistan, Afghanistan and Russia. Since the first detection of CCHF cases in Turkey in 2002, more than 9700 patients have been reported, with an overall mort...
journal_title：Antiviral research
pub_type： 历史文章,杂志文章,评审
doi：10.1016/j.antiviral.2015.12.003
更新日期：2016-02-01 00:00:00
abstract：:Drug resistance testing has proven its use to guide treatment decisions in HIV-1 infected patients. Genotyping is the preferred technique for clinical drug resistance testing. Many factors complicate the interpretation of mutations towards therapy response, such that an interpretation system is necessary to help the c...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/j.antiviral.2006.05.003
更新日期：2006-09-01 00:00:00
abstract：:A novel substituted naphthalenone (TGG-II-23A) has been found that inhibits HIV-1 infection of CEM-SS cells at concentrations that are not cytotoxic. Time of addition experiments indicate that TGG-II-23A functions at a stage of the HIV-1 life cycle at or near reverse transcription. Cell free assays confirmed that TGG-...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(93)90091-v
更新日期：1993-10-01 00:00:00
abstract：:IRES-driven translation plays an essential role in picornavirus infection. However, there are seldom reports of compounds targeting this pathway with effective protection in animal models. Here, we identified emetine, an antiprotozoal drug, which inhibits EV-A71 with an EC50 value of 0.04 μM and a CC50 value of 10 μM ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.104650
更新日期：2020-01-01 00:00:00
abstract：:Using several herbal extracts, we investigated whether certain Kampo medicines exert an inhibitory effect on the acidification of intracellular compartments such as endosomes and lysosomes (referred to as ELS), and thereby inhibit the growth of influenza A virus in Madin-Darby canine kidney cells. The vital fluorescen...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(99)00067-4
更新日期：1999-12-31 00:00:00
abstract：:Highly pathogenic influenza viruses pose a serious public health threat to humans. Although vaccines are available, antivirals are needed to efficiently control disease progression and virus transmission due to the emergence of drug-resistant viral strains. In this study, germacrone, which is a major component of the ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2013.09.021
更新日期：2013-12-01 00:00:00
abstract：:Imexon (4-imino-1,4-diazobicyclo-3.1.0-hexan-2-one) was moderately effective in the treatment of a retroviral infection in a genetically defined murine model. The animal model consisted of a Friend virus complex (FV) infection in a hybrid mouse strain, (B10.A x A/WySn)F1, which has similarities with acquired immune de...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(91)90040-x
更新日期：1991-01-01 00:00:00
abstract：:The essential role of SMAR1 in HIV-1 transcription and LTR driven gene expression suggests SMAR1 as an HIV dependency factor (HDF) and a potential anti-HIV therapeutic target. Here, we report for the first time, anti-HIV activity of 8 novel isothiocyanate (ITC) derivatives that differentially stabilise SMAR1. Out of 8...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.104648
更新日期：2020-01-01 00:00:00
